Activation specific inhibitors of nf-kb and method of treating inflammatory processes in cardio-vascular diseases

Abstract

A 5H-Thiazolo[3,2]pyrimidine derivative or a salt thereof for use as a medicine, which is represented by the following formula (A): wherein R represents an optionally substituted phenyl or pyridyl group; R4 represents a hydroxyl group, an amino group, a straight chain or branched alkoxy group, a straight chain or branched alkyl group, a cycloalkyloxy group, an alkylamino group, a cycloalkylamino group, a dialkylamino group, R 5 represents a hydrogen atom, a straight chain or branched alkyl group, R 6 and R 7 , which may be the same or different represent a hydrogen atom, a halogen atom, a straight chain or branched alkyl group, a straight chain or branched alkoxy group, a straight chain or branched alkenyl group, a cycloalkyl group, an aryl group, X, Y, and Z which may be same or different represent a hydrogen atom, a halogen atom, a carboxyl group a nitro group, a cyano group, an alkyl group, an alkoxy group or an acyl group.

1 - 47 . (canceled)  
   
   
       48 . A 5H-Thiazolo[3,2]pyrimidine derivative or a salt thereof for use as a medicine, which is represented by the following formula (B):  
     
       
         
         
             
             
         
       
       wherein  
       the dotted lines independently represent a single bond or a double bond,  
       R represents an optionally substituted phenyl or pyridyl group  
       R 4  represents 
 a hydroxyl group,  
 an amino group,  
 a straight chain or branched alkoxy group,  
 a straight chain or branched alkyl group,  
 a cycloalkyloxy group,  
 an alkylamino group,  
 a cycloalkylamino group,  
 a dialkylamino group;  
 
       R 5  represents 
 a hydrogen atom,  
 
       a straight chain or branched alkyl group,  
       X 1  represents O, S, or NH;  
       X, Y, and Z which may be same or different represent 
 a hydrogen atom,  
 a halogen atom,  
 a carboxyl group  
 a nitro group,  
 a cyano group,  
 an alkyl group,  
 an alkoxy group or  
 an acyl group.  
 
     
   
   
       49 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt thereof according to  claim 48 , wherein the dotted lines in formula (B) are both double bonds.  
   
   
       50 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt thereof according to  claim 48 , wherein R represents a substituted phenyl group.  
   
   
       51 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt thereof according to  claim 48 , wherein R 4  represents a straight chain or branched alkoxy group.  
   
   
       52 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt thereof according to  claim 48 , wherein R 5  represents a straight chain or branched alkyl group.  
   
   
       53 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt thereof according to claims  48 , wherein X 1  represents O.  
   
   
       54 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt thereof according to  claim 48 , wherein X, Y, and Z which may be same or different represent a hydrogen atom or a carboxyl group, or a salt thereof.  
   
   
       55 . COM 56 of  FIG. 7  including any geometric isomer regarding the exocyclic double bond.  
   
   
       56 . A 5H-Thiazolo[3,2]pyrimidine derivative or a salt or ester thereof for use as a medicine, which is represented by the following formula (II):  
     
       
         
         
             
             
         
       
       wherein  
       R 1  and R 2  which may be the same or different, represent 
 a straight chain or branched alkyl group,  
 a straight chain or branched alkenyl group,  
 a cycloalkyl group,  
 an aryl group, or  
 R 1  and R 2  together may form an alkylene group;  
 
       R 3  represents 
 a hydrogen atom,  
 a halogen atom,  
 a straight chain or branched alkyl group,  
 
       R 4  represents 
 a straight chain or branched alkoxy group,  
 a straight chain or branched alkyl group,  
 a cycloalkyloxy group,  
 an alkylamino group,  
 a cycloalkylamino group,  
 
       R 5  represents 
 a hydrogen atom,  
 a straight chain or branched alkyl group,  
 
       X, Y, and Z which may be same or different represent 
 a hydrogen atom,  
 a carboxyl group  
 a halogen atom,  
 a nitro group,  
 a cyano group, or  
 an acyl group.  
 
     
   
   
       57 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt or ester thereof for use as a medicine according to  claim 56 , wherein R 1  and R 2  are the same or different and represent an alkyl group or together form an alkylene group.  
   
   
       58 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt or ester thereof for use as a medicine according to  claim 56 , wherein R 3  represents a halogen atom.  
   
   
       59 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt or ester thereof for use as a medicine according to  claim 56 , wherein R 4  represents a straight chain or branched alkoxy group.  
   
   
       60 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt or ester thereof for use as a medicine according to  claim 56 , wherein R 5  represents a straight chain or branched alkyl group.  
   
   
       61 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt or ester thereof for use as a medicine according to  claim 56 , wherein X is a carboxyl group and Y and Z represent a hydrogen atom.  
   
   
       62 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt or ester thereof for use as a medicine according to  claim 56  wherein the phenyl or pyridyl group represented by R is substituted by 1 to 3 substituents selected from the group consisting of a halogens such as fluorine, chlorine, bromine and iodine, a cyano group, a hydroxy group, a nitro group, a carboxyl group, an amino group, a straight chain or branched C 1-6  alkyl group, a straight chain or branched C 1-6  alkoxy group, a straight chain or branched C 1-7  alkylcarbonyl group, a straight chain or branched C 1-7  alkoxycarbonyl group, straight chain or branched C 1-7  alkoxycarbonyloxy group, a straight chain or branched C 1-6 alkylamino group, a straight chain or branched di-C 1-6 alkylamino group, a straight chain or branched C 1-7  alkylcarbonylamino group, a straight chain or branched C 1-6 alkylaminocarbonyl group, a straight chain or branched C 1-7  alkoxycarbonylamino group, a straight chain or branched C 1-7  alkylaminocarbonyloxy group.  
   
   
       63 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt or ester thereof for use as a medicine according to  claim 61 , wherein R is a phenyl group.  
   
   
       64 . The 5H-Thiazolo[3,2]pyrimidine derivative or a salt or ester thereof for use as a medicine according to  claim 62 , wherein 1 to 3 substituents a present which are selected from a halogen atom or an alkoxy group.  
   
   
       65 . A pharmaceutical composition comprising the compound according to  claim 48  as an active ingredient.  
   
   
       66 . A method for the treatment or prevention of inflammatory diseases, which comprises the step of administering to a patient a compound according to  claim 48 .  
   
   
       67 . The method according to  claim 66 , wherein the inflammatory disease is atherosclerosis.